Alkyl Urea NAMPT Modulators for NAD+ Biosynthesis
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current strategies to boost NAD+ levels are inadequate for effectively addressing a broad spectrum of diseases, including cardiac, metabolic, neurological, and age-related conditions, as they fail to efficiently modulate nicotinamide phosphoribosyltransferase (NAMPT) activity.
Innovation Solution
Development of alkyl urea compounds that modulate NAMPT activity, enhancing NAD+ biosynthesis by acting as NAMPT activators, thereby increasing cellular NAD+ levels to treat various diseases and conditions mediated by NAMPT.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current strategies to boost NAD+ levels are used, then some therapeutic effect is achieved, but they fail to efficiently modulate NAMPT activity and address a broad spectrum of diseases
Solution Approach 1:
The patent employs parameter changes by developing alkyl urea compounds with specific molecular structures (Formula I and Formula II) that optimize NAMPT activation. The compounds feature variable parameters including R1-R6 substituents, n values (0-6), and Y1 groups, allowing fine-tuning of NAMPT modulation efficiency to achieve both reliable therapeutic effects and broad disease coverage
Solution Approach 2:
The invention achieves universality by creating a single class of compounds (alkyl urea NAMPT activators) that can effectively treat multiple disease types including cardiac, metabolic, neurological, and age-related conditions. The compounds serve multiple therapeutic functions across different disease states through their ability to broadly enhance NAMPT activity and increase cellular NAD+ levels
2Productivity
If alkyl urea compounds are developed to modulate NAMPT activity, then NAD+ biosynthesis is enhanced, but compound complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the complex molecular structure into distinct functional segments: the core alkyl urea moiety (Formula I or II), variable R1-R6 substituent groups, and optional Y1 attachments. This modular segmentation allows systematic optimization of NAD+ biosynthesis enhancement while managing structural complexity through defined compositional elements
Solution Approach 2:
The invention uses local quality by assigning specific functional properties to different parts of the molecule. The core alkyl urea structure provides NAMPT activation, while specific R groups (such as R3 as aryl or heteroaryl, R4 as phenyl) provide targeted molecular recognition and binding properties, allowing optimization of NAD+ production efficiency without excessive overall complexity
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The alkyl urea compounds effectively increase NAD+ levels, providing a therapeutic approach to prevent or treat multiple disease states by enhancing NAMPT activity, thereby addressing the limitations of existing strategies.
Implementation Method 1
alkyl urea compounds that modulate NAMPT activity, enhancing NAD+ biosynthesis by acting as NAMPT activators
Data Source
AI summary
Provided are compounds of Formula (II): or a pharmaceutically acceptable salt thereof, wherein R1, n, and Y1 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.